Bexarotene-LGD1069-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBexaroteneCat.No.:HY-14171CASNo.:153559-49-0Synonyms:LGD1069分⼦式:C₂₄H₂₈O₂分⼦量:348.48作⽤靶点:RAR/RXR;Autophagy作⽤通路:MetabolicEnzyme/Protease;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:60mg/mL(172.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8696mL14.3480mL28.6961mL5mM0.5739mL2.8696mL5.7392mL10mM0.2870mL1.4348mL2.8696mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.97mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.97mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.97mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:2.62mg/mL(7.52mM);Suspendedsolution;Needultrasonic5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.62mg/mL(7.52mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Bexarotene(LGD1069)⼀种⾼亲和⼒的选择性类视醇X受体(RXR)激动剂，对RXRα、RXRβ和RXRγ的EC50分别为33、24、25nM。Bexarotene对RAR受体的亲和⼒有限(EC50>10000nM)[1][2][3]。Bexarotene可⽤于⽪肤T细胞淋巴瘤的研究。体外研究BexaroteneselectivelybindsandactivatesRXRsubtypeswithKd=14±2nM,21±4nM,and29±7nMforRXRα,RXRβ,andRXRγsubtypes[1].Bexaroteneiseffectiveinlimitingtheproliferationofleukemic(HL-60)cells.BexaroteneinhibitstheproliferationofHL-60cellsby37%at1μM[1].Bexarotenemonotherapyofcellsshowsanantiproliferativeeffectatahighdose,andtheIC50saere40.62±0.45µM(PC3)and50.20±4.10µM(DU145)[2].Bexarotene(20and40µM)andDocetaxel(5and10µM)exhibitasynergisticeffectontheinhibitionofPC3andDU145cellproliferation[2].Bexarotene(20and40µM)repressescyclinD1andcyclinD3expressioninPC3andDU145cells[2].CellProliferationAssay[2]CellLine:ThehumanPCaandrogen-independentcelllinesPC3andDU145Concentration:5,10,20,30,40μMforPC3cells;1,5,10,20,40μMforDU145cells.IncubationTime:24and48hoursResult:ShowedanantiproliferativeeffectwiththeIC50swere40.62±0.45µM(PC3)and50.20±4.10µM(DU145).CellViabilityAssay[2]CellLine:PC3andDU145cellsConcentration:20and40µMIncubationTime:24or48hours2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:DecreasedcyclinD1,andcyclinE2after24hourstreatment.NotonlydecreasedtheexpressionofcyclinD1andcyclinE2butrepressedcyclinB1andCDK1expressionafter48hourstreatment.体内研究Bexarotene(1mg/kg/day)iseffectiveinblockingthedevelopmentofbehavioraldeficitsanddopamineneurondegenerationinaratmodelofParkinson’sdisease(PD)producingsignificantlyreducedchangesinbothtriglyceridesandT4serum[1].Bexaroteneisaneffectivepreventiveagentagainstlungtumorgrowthandprogression.Bexarotene((100ꢀmg/kgbygavage)inhibitsbothtumormultiplicityandtumorvolumeinmiceofallthreegenotypes(p53wt/wtK-raswt/wt,p53val135/wtK-raswt/wt,orp53wt/wtK-rasko/wt).Bexarotenereducestheprogressionofadenomatoadenocarcinomaby-50%inbothp53wt/wtK-rasko/wtandp53wt/wtK-raswt/wtmice[3].AnimalModel:UL53-3mice(p53wt/wtK-raswt/wt,p53val135/wtK-raswt/wt,orp53wt/wtK-rasko/wt)[3]Dosage:100ꢀmg/kgAdministration:Gavagewith18gageofgavage-needle,0.1ꢀmLpermouseperday,5timesaweek,continuedfor12weeksResult:Inhibitedbothtumormultiplicityandtumorvolumeinmiceofallthreegenotypes.户使⽤本产品发表的科研⽂献•Cell.2018Aug9;174(4):843-855.e19.•JMedChem.2022Jan21.•IntJBiolMacromol.2022Feb1;204:144-153.•Cells.2022,11(17),2633.•NeurobiolDis.2018Sep;117:114-124.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NathaliaRodriguesdeAlmeida,etal.AreviewofthemoleculardesignandbiologicalactivitiesofRXRagonists.MedResRev.2019Jul;39(4):1372-1397.[2].DanyangShen,etal.SynergisticeffectofaretinoidXreceptor-selectiveligandbexaroteneanddocetaxelinprostatecancer.OncoTargetsTher.2019Sep24;12:7877-7886.[3].YWang,etal.Preventionoflungcancerprogressionbybexaroteneinmousemodels.Oncogene.